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Assay Detail

CHEMBL4052942

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Binding
Inhibition of NIK (unknown origin) after 1 to 2 hrs by ADP-FP assay
30
Total Activities
30
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Binding
Organism Homo sapiens
Confidence 9 — Direct single protein target
Curated By Autocuration

Target

Mitogen-activated protein kinase kinase kinase 14 (CHEMBL5888)
Type SINGLE PROTEIN
Organism Homo sapiens

Publication

Structure-Based Design of Tricyclic NF-κB Inducing Kinase (NIK) Inhibitors That Have High Selectivity over Phosphoinositide-3-kinase (PI3K).
Castanedo GM, Blaquiere N, Beresini M, Bravo B, Brightbill H, Chen J, Cui HF, Eigenbrot C, Everett C, Feng J, Godemann R, Gogol E, Hymowitz S, Johnson A, Kayagaki N, Kohli PB, Knüppel K, Kraemer J, Krüger S, Loke P, McEwan P, Montalbetti C, Roberts DA, Smith M, Steinbacher S, Sujatha-Bhaskar S, Takahashi R, Wang X, Wu LC, Zhang Y, Staben ST.
J Med Chem (2017) 60 : 627 -640
PubMed 28005357 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
Ki 30 7.57 9.52

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4098056 1 9.52
CHEMBL4073390 1 9.40
CHEMBL3692450 1 9.33
CHEMBL3696566 1 9.10
CHEMBL3692496 1 8.82
CHEMBL3692396 1 8.70
CHEMBL4065087 1 8.54
CHEMBL3692493 1 8.52
CHEMBL3692485 1 8.49
CHEMBL3692400 1 8.15
CHEMBL3692380 1 8.12
CHEMBL3692429 1 8.06
CHEMBL3696573 1 8.00
CHEMBL3692529 1 7.70
CHEMBL3692374 1 7.70
CHEMBL3692360 1 7.55
CHEMBL3692389 1 7.45
CHEMBL3692362 1 7.44
CHEMBL3692382 1 7.40
CHEMBL3692391 1 7.39
CHEMBL3692369 1 7.00
CHEMBL3692388 1 6.70
CHEMBL3692359 1 6.51
CHEMBL3696567 1 6.39
CHEMBL3696549 1 6.26
CHEMBL3692406 1 6.01
CHEMBL3696550 1 5.93
CHEMBL4086137 1 5.89
CHEMBL3692405 1 5.60
CHEMBL3692412 1 5.37

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4098056 Ki = 0.3 nM 9.52
CHEMBL4073390 Ki = 0.4 nM 9.40
CHEMBL3692450 Ki = 0.47 nM 9.33
CHEMBL3696566 Ki = 0.8 nM 9.10
CHEMBL3692496 Ki = 1.5 nM 8.82
CHEMBL3692396 Ki = 2.0 nM 8.70
CHEMBL4065087 Ki = 2.9 nM 8.54
CHEMBL3692493 Ki = 3.0 nM 8.52
CHEMBL3692485 Ki = 3.2 nM 8.49
CHEMBL3692400 Ki = 7.0 nM 8.15
CHEMBL3692380 Ki = 7.5 nM 8.12
CHEMBL3692429 Ki = 8.7 nM 8.06
CHEMBL3696573 Ki = 9.9 nM 8.00
CHEMBL3692529 Ki = 20.0 nM 7.70
CHEMBL3692374 Ki = 20.2 nM 7.70
CHEMBL3692360 Ki = 28.0 nM 7.55
CHEMBL3692389 Ki = 35.5 nM 7.45
CHEMBL3692362 Ki = 36.0 nM 7.44
CHEMBL3692382 Ki = 40.0 nM 7.40
CHEMBL3692391 Ki = 41.0 nM 7.39
CHEMBL3692369 Ki = 101.0 nM 7.00
CHEMBL3692388 Ki = 201.0 nM 6.70
CHEMBL3692359 Ki = 310.0 nM 6.51
CHEMBL3696567 Ki = 405.0 nM 6.39
CHEMBL3696549 Ki = 547.0 nM 6.26
CHEMBL3692406 Ki = 986.0 nM 6.01
CHEMBL3696550 Ki = 1164.0 nM 5.93
CHEMBL4086137 Ki = 1280.0 nM 5.89
CHEMBL3692405 Ki = 2503.0 nM 5.60
CHEMBL3692412 Ki = 4282.0 nM 5.37